Ceccaldi Pierre-Francois, Ferreira Claudia, Gavard Laurent, Gil Sophie, Peytavin Gilles, Mandelbrot Laurent
Department of Obstetrics and Gynecology, Louis Mourier Hospital, Assistance Publique-Hôpitaux de Paris, and Paris 7-Denis Diderot University, Paris, France.
Am J Obstet Gynecol. 2008 Apr;198(4):433.e1-2. doi: 10.1016/j.ajog.2007.10.802. Epub 2008 Feb 1.
The objective of the study was to determine the placental transfer of the antiretroviral fusion inhibitor, enfuvirtide (Fuzeon).
Human cotyledons were perfused for 90 minutes in an open dual circuit with enfuvirtide, and fetal venous samples were collected every 5 minutes. Three perfusion experiments were validated using antipyrine.
Enfuvirtide was not detected in the fetal compartment in any of the 3 experiments. The mean concentration of the drug measured in the maternal compartment was 12,400 ng/mL (range, 6500-16,200 ng/mL), which is 2.5 times the maximum concentration recommended for patients treated with enfuvirtide.
Even at maternal concentrations twice above therapeutic levels, no placental transfer of enfuvirtide was observed. The high molecular weight of the molecule (4492 kDa) and its ionized state may account for the lack of placental transfer. This result suggests that enfuvirtide could be used in HIV-infected pregnant women without causing fetal exposure.
本研究的目的是确定抗逆转录病毒融合抑制剂恩夫韦肽（Fuzeon）的胎盘转运情况。
在开放双循环中用恩夫韦肽对人胎盘小叶灌注90分钟，每5分钟采集一次胎儿静脉样本。使用安替比林对三个灌注实验进行验证。
在3个实验中的任何一个中，胎儿隔室均未检测到恩夫韦肽。在母体隔室中测得的药物平均浓度为12400 ng/mL（范围为6500 - 16200 ng/mL），这是恩夫韦肽治疗患者推荐最大浓度的2.5倍。
即使母体浓度高于治疗水平两倍，也未观察到恩夫韦肽的胎盘转运。该分子的高分子量（4492 kDa）及其离子化状态可能是胎盘转运缺乏的原因。这一结果表明，恩夫韦肽可用于感染HIV的孕妇而不会导致胎儿暴露。
